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Applied Biopharmaceutics & Pharmacokinetics, Sixth Edition

Applied Biopharmaceutics and Pharmacokinetics

Summary

The most comprehensive text on the practical applications of biopharmaceuticals and pharmacokinetics! The required text for the biopharmaceuticals and/or pharmacokinetics course sequence, this text emphasizes the application and understanding of concepts. Thoroughly revised, this edition continues to help students gain skills in problem solving and features examples, practice problems, and solutions.

Author Biography

Leon Shargel, PhD is vice president of biopharmaceutics at Eon Labs, Inc. Wilson, NC., Susanna Wu-Pong, PhD, RPh is an associate professor in the department of pharmaceutics at Virginia Commonwealth University, Richmond, Virginia, Andrew B.C. Yu,PhD, RPh, formerly a professor at the Albany College of Pharmacy, is currently with the FDA in Rockville, MD.

Table of Contents

Preface

xv

Glossary

xvii

1. INTRODUCTION TO BIOPHARMACEUTICS AND PHARMACOKINETICS

1

(20)

Biopharmaceutics

1

(2)

Pharmacokinetics

3

(1)

Clinical Pharmacokinetics

3

(1)

Pharmcodynamics

4

(1)

Toxicokinetics and Clinical Toxicology

4

(1)

Measurement of Drug Concentrations

5

(4)

Basic Pharmacokinetics and Pharmacokinetic Models

9

(9)

References

18

(1)

Bibliography

18

(3)

2. MATHEMATIC FUNDAMENTALS IN PHARMACOKINETICS

21

(30)

Math Self-Exam

21

(1)

Estimation and the Use of Calculators and Computers

22

(5)

Calculus

27

(3)

Graphs

30

(7)

Units in Pharmacokinetics

37

(1)

Measurement and Use of Significant Figures

38

(1)

Units for Expressing Blood Concentrations

39

(1)

Statistics

39

(3)

Rates and Orders of Reactions

42

(5)

Frequently Asked Questions

47

(1)

Learning Questions

48

(2)

References

50

(1)

Bibliography

50

(1)

3. ONE-COMPARTMENT OPEN MODEL: INTRAVENOUS BOLUS ADMINISTRATION

51

(22)

Elimination Rate Constant

52

(1)

Apparent Volume of Distribution

53

(4)

Clearance

57

(6)

Calculation of K from Urinary Excretion Data

63

(6)

Frequently Asked Questions

69

(1)

Learning Questions

69

(3)

Reference

72

(1)

Bibliography

72

(1)

4. MULTICOMPARTMENTAL MODELS: INTRAVENOUS BOLUS ADMINISTRATION

73

(32)

Two-Compartment Open Model

75

(18)

Three-Compartment Open Model

93

(2)

Determination of Compartment Models

95

(6)

Frequently Asked Questions

101

(1)

Learning Questions

102

(3)

References

105

(1)

Bibliography

105

(1)

5. INTRAVENOUS INFUSION

105

(26)

One-Compartment Model Drugs

108

(4)

Infusion Method for Calculating Patient Elimination Half-Life

112

(3)

Loading Dose Plus IV Infusion: One-Compartment Model

115

(7)

Estimation of Drug Clearance and VD from Infusion Data

122

(1)

Intravenous Infusion of Two Compartment Model Drugs

122

(1)

Loading Dose Plus IV Infusion: Two-Compartment Model

123

(4)

Frequently Asked Questions

127

(1)

Learning Questions

127

(2)

Reference

129

(1)

Bibliography

129

(2)

6. DRUG ELIMINATION AND CLEARANCE

131

(30)

Drug Elimination

131

(1)

The Kidney

132

(4)

Renal Drug Excretion

136

(3)

Drug Clearance

139

(3)

Clearance Models

142

(2)

Renal Clearance

144

(5)

Determination of Renal Clearance

149

(6)

Relationship of Clearance to Elimination Half-Life and Volume of Distribution

155

(2)

Frequently Asked Questions

157

(1)

Learning Questions

158

(1)

References

159

(1)

Bibliography

159

(2)

7. PHARMACOKINETICS OF ORAL ABSORPTION

161

(24)

Pharmacokinetics of Drug Absorption

161

(2)

Zero-Order Absorption Model

163

(1)

First-Order Absorption Model

164

(17)

Significance of Absorption Rate Constants

181

(1)

Frequently Asked Questions

182

(1)

Learning Questions

182

(2)

References

184

(1)

Bibliography

184

(1)

8. MULTIPLE DOSAGE REGIMENS

185

(34)

Drug Accumulation

185

(5)

Repetitive Intravenous Injections

190

(7)

Intermittent Intravenous Infusion

197

(4)

Estimation of k and VD of Aminoglycosides in Clinical Situations

201

(1)

Multiple-Oral-Dose Regimen

202

(3)

Loading Dose

205

(2)

Determination of Bioavailability and Bioequivalance in a Multiple-Dose Regimen